Synthesis method of amikacin
The invention discloses a synthesis method of amikacin. The synthesis method comprises following steps: firstly, a partially silanization protection product of kanamycin A is prepared; dehydration of the partially silanization protection product with PHBA under the action of DCC is carried out so as...
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Format: | Patent |
Sprache: | chi ; eng |
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Zusammenfassung: | The invention discloses a synthesis method of amikacin. The synthesis method comprises following steps: firstly, a partially silanization protection product of kanamycin A is prepared; dehydration of the partially silanization protection product with PHBA under the action of DCC is carried out so as to obtain a acylated product; the acylated product is subjected to hydrolysis, nitrilase, and column chromatography purification so as to obtain amikacin. According to the synthesis method, NOP is not used, synthesis of an active ester via esterification is avoided, damage on the health of workers is reduced greatly, solid waste generated in production process is reduced greatly, product yield is increased, and the synthesis method is especially suitable for industrialized production.
本发明公开了种阿米卡星的合成方法。该合成方法为:首先制备卡那霉素A的部分硅烷化保护产物;然后将其与PHBA在DCC作用下脱水,得到酰化产物;酰化产物经水解、腈解反应以及柱层析提纯得到阿米卡星。本发明的合成方法不再使用NOP,去掉了现有专利报道的酯化合成活性酯步骤,大幅降低对职工健康的损害;而且生产过程产生的固体废弃物可大幅减少,产品收率提高,非常适合工业化生产。 |
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